Chapter 3: Adrenergic Pharmacology

Question 1

What is the main way NE leaves synaptic cleft?

Answer 1

through NE reuptake

Question 2

What is the main transporter by which NE reuptaken?

Answer 2

through NaCl - NE co-transporter driven by the sodium gradient and maintained by Na+/K+ ATPase

Question 3

Where are a1 receptors found and what do they do?

Answer 3

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Question 4

Where are the a2 receptors located and what is the response?

Answer 4

Question 5

Where are the B1 receptors located and what is their response?

Answer 5

Question 6

Where are the B2 receptors located and what is their response?

Answer 6

Question 7

Where are the B3 receptors located and what is their response?

Answer 7

Question 8

Where are the D1 (peripheral) located and what is their response?

Answer 8

Question 9

Which cells mediate release of renin from kidneys via B1 activation?

Answer 9

JG cells

Question 10

Fenoldopam use and MOA.

Answer 10

D1 agonist used for severe hypertension

Question 11

DA can affect which adrenergic receptors. (List from most affected by lower doses to higher doses)

Answer 11

D1

B1

a1

Question 12

What G-protein coupled receptor pathway does a1 follow?

Answer 12

Gq > increased phospholipase C > IP3, DAG > inc. Ca 2+

Question 13

What G protein coupled receptor pathway does a2 follow?

Answer 13

Gi coupled

Gi> dec adenylyl cyclase > dec. cAMP

Question 14

What G-protein receptor pathway does B1 follow?

Answer 14

Gs
inc adenylyl cyclase > inc. cAMP

Question 15

What G protein coupled receptor pathway does B2 follow?

Answer 15

inc adenylyl cyclase > inc. cAMP

Question 16

What G protein coupled receptor pathway does D1 follow?

Answer 16

inc adenylyl cyclase > inc. cAMP

Question 17

Clinical use of phenylephrine.

Answer 17

nasal decongestant and ophthalmologic use (mydriasis without cyclopegia), hypotensive states

Question 18

MOA of phenylephrine.

Answer 18

a1 agonist

Question 19

What are the prototype a2 agonist?

Answer 19

E=MC2
methyldopa
clonidine

Question 20

What are the β agonist drugs we discussed?

Answer 20

• Isoproterenol (β1=β2)
• Dobutamine ( β1> β2) congestive heart failure CHF
• Selective β2 agonists: salmeterol, albuterol, terbutaline (asthma and premature labor)
• Selective β3 agonist: mirabegron (overactive bladder)

Question 21

What are the mixed receptor acting adrenergic agonist neurotransmitters?

Answer 21

NE and Epi

Question 22

Trick to remember some selective Beta2 agonists?

Answer 22

terol for B2 agonists

Question 23

What are the effects of epinephrine on BP and HR?

Answer 23

depends on dose

low dose mimics isopreteronol
high dose mimics NE

Question 24

How would you distinguish between isoproterenol and Epi on a trace diagram?

Answer 24

if gave more of the dose then graph would change unlike in isoproterenol in which it would not change

Question 25

How do you differentiate between high dose Epi and NE.

Answer 25

Administer alpha blocker In NE if do this the BP returns do baseline In Epi BP won't return to baseline because of B2 activity

Question 26

Some metabolic effects of B2 agonists?

Answer 26

increased glycogenolysis (muscle and liver) inc. gluconeogenesis mobilization of fat

Question 27

What are some major uses of NE and Epi?

Answer 27

* cardiac arrest because of B1 benefit * adjunct to local anesthetics because of epi a1 benefit * hypotension because of a1 benefit * anaphylaxis (epi only) strong B2 benefit * Asthma (mostly epi used) B2 benefit

Question 28

Name some indirect acting adrenergic receptor agonists considered releasers.

Answer 28

tyramine amphetamines pseudoephedrine

Question 29

Clinical use of pseudoephedrine?

Answer 29

cold medication

Question 30

Clinical use amphetamines like methylphenidate?

Answer 30

narcolepsy and ADHD

Question 31

If given an MAO-A inhibitor what should a patient not eat?

Answer 31

red wine, cheese

Question 32

MAO type A found mainly where? What does it metabolize?

Answer 32

liver but Anywhere NE, 5HT and tyramine

Question 33

Where is MAO type B found? What does it metabolize?

Answer 33

Brain Metabolizes DA

Question 34

Name some reuptake inhibitors that are indirect-acting adrenergic receptor agonists?

Answer 34

cocaine tricyclic antidepressants

Question 35

Major uses of alpha receptor antagonist?

Answer 35

HTN pheochromocytoma (use of nonselective a blocker to control BP before surgery) BPH: selective a1 blocker

Question 36

List drugs considered non-selective alpha receptor antagonist.

Answer 36

phentolamine (competitive inhibitor) phenoxybenzamine (noncompetitive inhibitor)

Question 37

List the drugs that are selective a1 blockers?

Answer 37

prazosin, doxazosin, terazosin, tamsulosin

Question 38

Trick to remember the selective a1 blockers?

Answer 38

"zosins" mostly

Question 39

MOA of tamsulosin? How does this pertain to clinical use? (benefits)

Answer 39

acts on alpha 1a receptor blockers; therefore only affects BPH not BP

Question 40

Which has the longer half-life? Phentolamine or phenoxybenzamine?

Answer 40

phenoxybenzamine

Question 41

B2 blockers have what metabolic effects?

Answer 41

block glycogenolysis, and gluconeogenesis inc. LDLs, TGs

Question 42

Reproduce this chart on Beta blockers

Answer 42

Question 43

How do you remember the B1 selective blockers?

Answer 43

A-M olol B1 selective N-Z olol B1 non selective

Question 44

How do you remember what is a B blocker and something else?

Answer 44

olol B blocker only ilol or alól B blocker and something else

Question 45

Carvedilol and labetalol have what adrenergic blocking activities?

Answer 45

alpha - 1 and B-blocking activity

Question 46

Clinical use of carvedilol and labetalol?

Answer 46

CHF and Hypertensive emergencies (respectively)

Question 47

Benefit of labetalol over carvedilol?

Answer 47

consistent decrease in HR.

Question 48

What is the mechanism of action of sotalol?

Answer 48

K+ channel blockade and B-blocking activity

Question 49

What are some general uses of beta- blockers?

Answer 49

angina, HTN, post-MI antiarrhythmics (class II: propranolol, acebutolol, esmolol) glaucoma (timolol) migraine, thyrotoxicosis, performance anxiety, essential tremor (propranolol)

Question 50

Yohimbine MOA and clinical use.

Answer 50

a2 antagonist postural hypotension

Question 51

Mirtazapine MOA?

Answer 51

a2 antagonist